Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-α-induced VCAM-1 expression

Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-α-induced VCAM-1 expression

Novel chalcone derivatives have been discovered as potent inhibitors of TNF-α-induced VCAM-1 expression. Thienyl or benzothienyl substitution at the meta-position of ring B helps boost potency while large substitution at the para-position on ring B is detrimental. Various substitutions are tolerated...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-03, Vol.14 (6), p.1513-1517
Hauptverfasser: Meng, Charles Q., Zheng, X.Sharon, Ni, Liming, Ye, Zhihong, Simpson, Jacob E., Worsencroft, Kimberly J., Hotema, Martha R., Weingarten, M.David, Skudlarek, Jason W., Gilmore, Joshua M., Hoong, Lee K., Hill, Russell R., Marino, Elaine M., Suen, Ki-Ling, Kunsch, Charles, Wasserman, Martin A., Sikorski, James A.
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Chalcone - chemistry
Chalcone - pharmacology
Heterocyclic Compounds - chemistry
Heterocyclic Compounds - pharmacology
Medical sciences
Pharmacology. Drug treatments
Tumor Necrosis Factor-alpha - antagonists & inhibitors
Tumor Necrosis Factor-alpha - pharmacology
Vascular Cell Adhesion Molecule-1 - biosynthesis
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Novel chalcone derivatives have been discovered as potent inhibitors of TNF-α-induced VCAM-1 expression. Thienyl or benzothienyl substitution at the meta-position of ring B helps boost potency while large substitution at the para-position on ring B is detrimental. Various substitutions are tolerated on ring A. A lipophilicity–potency relationship has been observed in several sub-series of compounds. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.01.021